josamycin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, produced by Streptomyces strains 1518 16846-24-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • josamycin
  • Leucomycin A3
  • iosalide
  • josacine
  • josamina
  • Turimycin A5
A macrolide antibiotic from Streptomyces narbonensis. The drug has antimicrobial activity against a wide spectrum of pathogens.
  • Molecular weight: 828.01
  • Formula: C42H69NO15
  • CLOGP: 3.67
  • LIPINSKI: 2
  • HAC: 16
  • HDO: 3
  • TPSA: 206.05
  • ALOGS: -4.19
  • ROTB: 14

Drug dosage:

DoseUnitRoute
2 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.320 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 15.740 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 12.078 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 30.832 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 23.240 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 30.930 % High 1
herg hERG pIC50 4.483 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 22.336 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 147.571 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 26.590 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1 19
kinase-selectivity-class MAP2K6 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 13.996 High 1
mh-clint Mouse hepatocyte intrinsic clearance 50.582 High 1
mppb Mouse plasma protein binding (% unbound) 18.920 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 29.785 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 24.030 % High 1
rh-clint Rat hepatocyte intrinsic clearance 71.450 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 62.670 % High 1
rppb Rat plasma protein binding (% unbound) 24.320 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 474.242 uM High 1

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01FA07 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS
Macrolides
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
CHEBI has role CHEBI:25212 metabolite
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:36047 antibacterial drug

Related Drugs by ATC class:

J01FA Macrolides 13 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.8 acidic
pKa2 13.95 acidic
pKa3 7.88 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
N0000168421 NUI
D01235 KEGG_DRUG
C0022419 UMLSCUI
CHEBI:31739 CHEBI
JOS PDB_CHEM_ID
CHEMBL224436 ChEMBL_ID
D015570 MESH_DESCRIPTOR_UI
DB01321 DRUGBANK_ID
12924 IUPHAR_LIGAND_ID
2837 INN_ID
HV13HFS217 UNII
5282165 PUBCHEM_CID
6084 RXNORM
005267 NDDF
713477009 SNOMEDCT_US

Pharmaceutical products:

None